A61K51/0472

IN VIVO STABLE HG-197(M) COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF IN NUCLEAR MEDICAL DIAGNOSTICS AND ENDORADIONUCLIDE THERAPY (THERANOSTICS)

The present invention relates to in vivo stable .sup.197(m)Hg compounds according to formula (E) for use in nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer, a method for the production of the .sup.197(m)Hg compounds comprising the step of radiolabeling of organic precursor compounds with NCA .sup.197(m)Hg by electrophilic substitution; and the use of the .sup.197(m)Hg compounds for nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer.

PSMA targeted fluorescent agents for image guided surgery

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

2,11-diaza-[3.3](2,6)pyridinophane compounds and their application as ligands of essential metal ion based MRI contrast agents and 52MN based PET contrast agents

The one subject of the invention is the compounds of general formula (I), their isomers, their physiologically acceptable salts and/or Mn(II), Fe(II), Fe(III), Co(II) and Ni(II) complexes. The other subject of the invention is the application of the above compounds. The compounds of general formula (I): wherein —NRR.sub.1 group may refer to: a) —NRR.sub.1 with N atom in the ring means a ring of 4 to 7, that in certain cases may contain another heteroatom, and in specific cases the ring may be replaced with an aryl group (of 5 to 7 carbon atoms) substituted with —COOH, —OH, —OCH.sub.3, —NO.sub.2, —NH.sub.2, —NCS, —NHS-activated ester, aryl (of 5 to 7 carbon atoms), or nitro-, amino- or isothiocyanate group, or b) in the —NRR.sub.1 group R means a H atom, alkyl, aryl, nitroaryl, aminoaryl or isothiocyanate-aryl group (of 1 to 6 carbon atoms) and R.sub.4 is a H atom, alkyl (of 1 to 6 carbon atoms) or —(CH.sub.2).sub.n—COOH group, whereas n=1 to 10 integer, or c) —NRR.sub.1 group is one of the following groups: (formula II) whereas R.sub.2 is a H atom, carboxyl- or alkyl-carbonyl group (of 1 to 4 carbon atoms); (formula III) and R.sub.2 is a H atom or alkyl or aryl group (of 1 to 6 carbon atoms), and X means independently from one another H atom, —CH.sub.3, —COOH, —OH, —OCH.sub.3, alkoxy- (of 2 to 6 carbon atoms), —NO.sub.2, —NH.sub.2, —NCS, —NHS-activated ester, alkyl (of 2 to 12 carbon atoms) or aryl (of 5 to 7 carbon atoms) group, in certain cases the latter may be substituted with hydroxyl, hydroxyalkyl (of 1 to 6 carbon atoms), nitro, amino or isothiocyanate group. ##STR00001##

Preparation of Metal-Pyridine Derivative Complexes for Use in Medical Imaging

The present invention relates to methods of forming metal-pyridine derivative complexes using pericyclic reactions with metal-1,2,4-triazine derivative complexes and a dienophile as the reactants. The reactants are bioorthogonal and the methods are particularly useful in preparing imaging agents.

PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY
20200216402 · 2020-07-09 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

KIT FOR LABELING A PROSTATE-SPECIFIC MEMBRANE ANTIGEN LIGAND WITH A RADIOACTIVE ISOTOPE
20200138985 · 2020-05-07 ·

A kit for labeling a prostate-specific membrane antigen (PSMA) ligand with a radioactive isotope such as .sup.68Ga, .sup.177Lu, or .sup.90Y. Radiolabeled PSMA ligands prepared by this kit can be used for both imaging and therapy purposes. The kit includes a disposable reaction vial containing predetermined amounts of a sodium-based buffering agent and a PSMA ligand, both in dried form; or two disposable reaction vials, wherein one of the reaction vials contains predetermined amounts of the sodium-based buffering agent in dried form and the other of the reaction vials that contains predetermined amounts of the PSMA ligand in dried form, wherein the reaction vial containing the PSMA ligand and optionally the sodium-based buffering agent further contains protons adhered to the inner walls of the reaction vial.

PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

LOADING OF HUMAN CAR T-CELLS WITH SUPERPARAMAGNETIC IRON-BASED PARTICLES FOR MAGNETIC TARGETING

The application describes a T-cell expressing a chimeric antigen receptor (CAR T-cell) containing superparamagnetic iron-based particles (loaded CAR T-cell) for use in treating a tumor. Said loaded CAR T-cell exhibits a reduced cytokine release upon binding to a cell of the tumor expressing an antigen being recognized by the CAR of the CAR T-cell, compared to a CAR T-cell not containing superparamagnetic iron-based particles (unloaded CAR T-cell) under the same conditions. Furthermore, an in vitro method of generating a CAR T-cell containing superparamagnetic iron-based particles is described, whereby such loaded CAR T-cells are generated.

LOADING OF HUMAN CAR T-CELLS WITH SUPERPARAMAGNETIC IRON-BASED PARTICLES FOR MAGNETIC TARGETING

The application describes a T-cell expressing a chimeric antigen receptor (CAR T-cell) containing superparamagnetic iron-based particles (loaded CAR T-cell) for use in treating a tumor. Said loaded CAR T-cell exhibits a reduced cytokine release upon binding to a cell of the tumor expressing an antigen being recognized by the CAR of the CAR T-cell, compared to a CAR T-cell not containing superparamagnetic iron-based particles (unloaded CAR T-cell) under the same conditions. Furthermore, an in vitro method of generating a CAR T-cell containing superparamagnetic iron-based particles is described, whereby such loaded CAR T-cells are generated.

PSMA targeted fluorescent agents for image guided surgery

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.